Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0016382 (flushing)
 6,387 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The efficacy of and tolerance to felodipine given as extended-release (ER) tablets once daily (o.d.) and the plain tablets twice daily (b.i.d.) were compared in this study. After a 4-week period on placebo and a beta-blocker, 102 patients who had a diastolic blood pressure (DBP) in the supine position greater than 95 mm Hg were randomized to treatment with felodipine ER tablets 10 mg o.d. (n = 50) or plain tablets 5 mg b.i.d. (n = 52). If the DBP was greater than 90 mm Hg after 2 weeks, the dose was doubled. The total treatment time on felodipine was 6 weeks. Blood pressure (BP) was measured 2 h after the dose and at the end of the dosing interval, i.e., 24 h after ER and 12 h after plain tablets. Both formulations reduced BP significantly (15/12 mm Hg in the ER and 13/11 mm Hg in the plain tablet group, at the end of the dosing interval). No differences in BP reduction were seen between the groups. The proportion of responders was 71% on ER and 65% on plain tablets 24 and 12 h, respectively, after dose intake, and greater than 90% in both groups, when measured 2 h after dose. Ankle swelling and flushing were the most frequently reported adverse events. Eight patients (three on ER) were withdrawn, most of them due to vasodilatory side effects. Felodipine ER once daily was as effective and tolerable as plain tablets b.i.d.
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PMID:Felodipine extended-release tablets once daily are equivalent to plain tablets twice daily in treating hypertension. Dutch Hospital Multicentre Group. 169 33

Felodipine is a dihydropyridine that blocks the slow entry channel for calcium. It is highly vascular selective and reduces blood pressure (BP) by dilatation of peripheral arterioles. It reduces BP in mild, moderate, and severe hypertension, and the fall in BP depends upon the initial level. It has been compared with a variety of other drugs as monotherapy or as add-on therapy. In these studies, felodipine (10-40 mg/day) has caused a similar or greater fall in BP and a similar or greater percentage of patients have achieved a diastolic BP less than or equal to 90 mm Hg. The plain tablet of felodipine needs to be given twice a day but an extended-release form can be given once daily. Some patients respond to 5 mg/day and most patients respond to a daily dose of 20 mg or less. The adverse effects are few except for a constellation of symptoms related to the vasodilator ability of the drug. These include palpitations, flushing, fatigue, dizziness, and headaches. These occur, if at all, usually within the first 2 weeks and diminish as the drug is continued. They can be limited by starting on a small dose of felodipine (5 mg/day). People who have these adverse effects usually have a good response to the drug. Another adverse effect, which is the most frequent reason for drug withdrawal, is ankle edema. This is more common on the higher doses of the drug. It is due to dilatation of the precapillary resistance vessels rather than sodium and water retention. Felodipine is a useful and effective antihypertensive drug and can be used as monotherapy or added to other antihypertensive drugs. It is effective in people with all grades of hypertension.
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PMID:A review of the antihypertensive effects of felodipine alone or in combination. 169 35

Hypertensive patients, particularly the elderly, may often suffer from other diseases. Therefore, antihypertensive compounds should not negatively affect such disorders. Felodipine is a calcium antagonist that has potentially beneficial effects in angina pectoris and congestive heart failure. Further, it does not adversely affect lung function in asthmatic patients or glucose tolerance in patients with diabetes. Preliminary investigations also indicate that felodipine has no negative influence on plasma lipid levels. Although felodipine seems to be safe in most patients, treatment with felodipine should at present be avoided in pregnant women, since digital anomalies have been observed in rabbit fetuses. The adverse effects seen during treatment with felodipine are usually mild and transient and generally related to the vasodilatory action of the drug, the most common being ankle edema, headache, flushing, dizziness, and palpitations. The only significant drug interactions with felodipine occur with inducers and inhibitors of the cytochrome P-450 system, which is responsible for the metabolism of felodipine.
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PMID:The safety of felodipine. 169 36

Felodipine, a dihydropyridine calcium-channel antagonist, significantly reduces systolic and diastolic blood pressure (BP) in patients with hypertension and has been associated with beneficial hemodynamic effects in patients with chronic stable angina pectoris or congestive heart failure (CHF). In hypertensive patients, felodipine does not appear to significantly affect glomerular filtration rate, creatinine clearance, glucose tolerance, or plasma lipoprotein concentrations. Studies comparing felodipine with other agents as monotherapy in mild to moderate hypertension have demonstrated felodipine to be at least as efficacious as hydrochlorothiazide (HCTZ) and HCTZ plus amiloride hydrochloride in combination. Comparisons of felodipine with other agents as adjuncts to beta-blocker or diuretic therapy have shown felodipine to be at least as effective as HCTZ, propranolol hydrochloride, prazosin hydrochloride, and nifedipine. Evaluations of patients with chronic stable angina are limited, and additional studies are needed before felodipine can be recommended for the routine management of angina pectoris. Similarly, additional studies are essential to delineate the role of felodipine, if any, in the management of CHF. In the management of hypertension, felodipine 5-40 mg/d significantly reduces systolic and diastolic BP. Although some patients may be controlled throughout the entire dosing interval when felodipine is administered bid, many patients will require more frequent dosing to obtain adequate BP control. Adverse effects associated with felodipine are similar to those of other dihydropyridine calcium-channel antagonists and include peripheral edema, headache, dizziness, flushing, and fatigue. A potentially clinically important drug interaction was observed when felodipine was administered concomitantly with theophylline aminopropanol; significant decreases in theophylline concentrations were noted. In summary, felodipine appears to be safe and effective for the management of hypertension when used alone or in combination with other antihypertensive agents. The efficacy of felodipine in the management of chronic stable angina pectoris and CHF requires further investigation.
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PMID:Felodipine: a new dihydropyridine calcium-channel antagonist. 176 37

Felodipine lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. The selective action may be considered a safeguard against untoward effects on cardiac contractility and conduction. Felodipine does not cause orthostatic hypotension since it has no effect in clinical doses on venous smooth muscle. Felodipine has a natriuretic/diuretic effect, which counteracts the salt and water retention that is often seen during treatment with other potent vasodilators. In clinical studies, felodipine has proved more effective than several established antihypertensive drugs. The combination of felodipine and a beta-adrenergic blocker appears to be a good alternative to standard triple treatment, and felodipine is often effective in patients with previously "refractory" hypertension. The antihypertensive effect of felodipine is dose related. In patients with moderate hypertension, a dose regimen of 5 mg twice a day is usually sufficient, and doses greater than 10 mg twice a day are not often required. Felodipine is generally well tolerated. The most common adverse effects are those expected from a potent arteriolar dilator: ankle swelling, headache, dizziness, flushing, etc. Adverse effects are usually transient or diminish in intensity with continued treatment. The overall frequency of adverse effects with felodipine appears to be similar to that for the established antihypertensive drugs, although the adverse effects differ. Felodipine is a potent arteriolar dilator with therapeutic advantages, especially for patients with moderate to severe hypertension.
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PMID:Felodipine in hypertension--a review. 244 9

Felodipine was compared with prazosin in patients with essential hypertension whose blood pressure was not controlled by a beta-blocking drug. One hundred patients with a supine diastolic blood pressure greater than or equal to mm Hg after 4 weeks or more on a beta-blocking drug and placebo were randomly assigned to felodipine or prazosin tablets. The drugs were titrated at 2-week intervals if diastolic BP was greater than or equal to 90 mm Hg. Titration steps of felodipine were 5, 10, 20 mg b.i.d. and of prazosin were 1, 2, 4 mg b.i.d. The fall in blood pressure with felodipine 32/21 mm Hg was greater than the fall with prazosin 16/12 mm Hg (p less than 0.001); 36 patients achieved a diastolic blood pressure of less than 90 mm Hg with felodipine, which was a significantly greater number than the 20 patients who obtained such a level with prazosin (p less than 0.01). Both drugs were well tolerated, but more patients complained of vascular type side effects (flushing, peripheral edema) with felodipine than with prazosin. There was significant weight gain with prazosin but not with felodipine. Felodipine was shown to be a well-tolerated, effective antihypertensive agent when used with a beta-blocking drug and to be suitable for people with hypertension who fail to be controlled with a beta-blocking drug.
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PMID:Felodipine compared to prazosin as additional therapy to a beta-blocking drug. 245 50

Although calcium antagonists may impair insulin release in vitro, clinical studies have produced conflicting results. Felodipine is a highly selective dihydropyridine calcium antagonist effective in the treatment of hypertension. The efficacy of felodipine was assessed in a double-blind randomized placebo cross-over study of 21 Type 2 diabetic patients with primary hypertension, 13 men and 8 women, with an age of 61 (range 46-73) years. Thirteen were controlled on oral hypoglycaemic therapy and 8 on diet alone. Mean (SD) blood pressure (mmHg) was 176(20)/102(8) after a 2-4 week placebo run-in period, 169(21)/101(8) during the subsequent placebo period compared with 151(15)/88(9) after 4 weeks felodipine therapy (p less than 0.001). Nineteen patients required 5 mg twice daily and 2 patients 10 mg twice daily to achieve a target diastolic pressure of 95 mmHg. Side-effects seen with felodipine included ankle oedema, facial flushing, headache, and dizziness. During oral glucose tolerance tests performed after the felodipine and placebo phases, mean (SD) fasting blood glucose was 9.5(3.1) and 9.0(3.0) mmol l-1, respectively (NS), and the 90 min (peak) blood glucose was 19.1(4.8) and 18.1(4.8) mmol l-1, respectively (NS). Glycosylated haemoglobin and fructosamine concentrations likewise showed no significant changes.
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PMID:A trial of the calcium antagonist felodipine in hypertensive type 2 diabetic patients. 253 42

24 hypertensive patients, who were not satisfactorily controlled (diastolic blood pressure greater than 95 mm Hg) with beta-blockers alone were randomised to 2 treatment groups where felodipine was administered for 2 weeks in a total daily dose of 15 mg divided in 2 or 3 doses. Following a 2-week placebo washout period, the patients were switched to the alternative dose regimen in a double-blind crossover manner. Blood pressure was measured with standard techniques and was also non-invasively monitored for 24 hours at the end of each dose regimen period and at the end of the intermediate placebo period. Mean arterial blood pressure at the end of the placebo run-in period was 169/105 mm Hg. Felodipine 5 mg thrice daily reduced blood pressure by 20/9 mm Hg and felodipine 7.5 mg twice daily by 17/9 mm Hg (p less than 0.05). The difference between the 2 dose regimens was not statistically significant. When 24-hour blood pressure measurements for the 2 dose regimens were compared, there were no statistically significant differences. Both regimens reduced the 24-hour blood pressure significantly compared with placebo. Two patients were withdrawn during the study, 1 before felodipine treatment started and the other due to diarrhoea and flushing related to felodipine. Otherwise felodipine was generally well tolerated.
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PMID:Antihypertensive effect of felodipine combined with beta-blockade. A comparison between 2 and 3 daily dosages. 285 85

In a placebo-controlled, double-blind, randomized, parallel group study one hundred and one patients with supine diastolic blood pressure greater than or equal to 100 mm Hg phase V, despite treatment with atenolol 100 mg plus chlorthalidone 25 mg once daily also received either felodipine 5-20 mg twice daily or hydralazine 25-100 mg twice daily for 6 weeks. Felodipine achieved a lower supine blood pressure (mean +/- s.d. 177/108 +/- 29/8-138/82 +/- 19/8 mm Hg) than hydralazine (174/109 +/- 25/8-149/92 +/- 26/11 mm Hg), (P less than 0.05/P less than 0.001). Felodipine also lowered supine diastolic blood pressure to less than 90 mm Hg more often than hydralazine (42 vs 22 patients, P less than 0.001). The incidence of unwanted effects was similar in both groups. The felodipine treated patients experienced more ankle swelling and flushing than those in the hydralazine group who experienced more headache and minor gastro-intestinal upset.
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PMID:Felodipine vs hydralazine: a controlled trial as third line therapy in hypertension. Cooperative Study Group. 287 21

The efficacy and tolerability of felodipine and prazosin were compared in a double-blind randomised parallel group study of 100 patients with moderately severe essential hypertension, treated concomitantly with a beta-blocking drug. After a 2- to 8-week run in phase (beta-blocking drug plus placebo), patients with a diastolic blood pressure greater than or equal to 95mm Hg were randomly given felodipine (n = 50) or prazosin (n = 50). After an initial dose of either felodipine 2.5mg bid or prazosin 0.5mg bid for 3 days, the drugs were titrated at 2-week intervals (felodipine 5, 10, 20mg bid, prazosin 1, 2, 4mg bid) if the supine diastolic blood pressure was greater than or equal to 90mm Hg. Treatment was continued for 8 weeks. Baseline supine blood pressures of each group were similar (177/104mm Hg, felodipine; 176/103mm Hg, prazosin). At week 6, supine blood pressures in the felodipine group were 144/82mm Hg and 161/90 in the prazosin group. The reductions in systolic and diastolic blood pressures were significantly greater for the felodipine group than the prazosin group in both the supine and standing positions at all visits after baseline. At 8 weeks, supine diastolic blood pressure less than 90mm Hg was achieved in more patients in the felodipine (36/47) than in the prazosin group (20/43, p less than 0.01). The total number of adverse reactions was similar in both groups. During active therapy, a greater number of patients experienced vascular adverse reactions (oedema and flushing) with felodipine (23) than with prazosin (12). Most events were mild and did not necessitate withdrawal from therapy. There were no clinically significant changes in laboratory variables in either treatment group. Felodipine was an effective, well tolerated hypotensive agent when used concomitantly with a beta-blocking drug. In the doses used it was more effective than prazosin at reducing blood pressure.
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PMID:Felodipine versus prazosin as an addition to a beta-blocker in the treatment of essential hypertension. The Australian Multicentre Study. 289 71


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